RETRACTED: Research progress of indole-fused derivatives as allosteric modulators: Opportunities for drug development

IDF Diabetes Atlas: Global estimates of diabetes prevalence for 2017 and projections for 2045

Cho, N. H., Shaw, J. E., Karuranga, S., Huang, Y., da Rocha Fernandes, J. D., Ohlrogge, A. W., & Malanda, B. (2018) · Diabetes Research and Clinical Practice · doi:10.1016/j.diabres.2018.02.023 · Cited by 7,283 · see citing works

Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain

Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527 · see citing works

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

Dixon, A. S., Schwinn, M. K., Hall, M. P., Zimmerman, K., Otto, P., Lubben, T. H., Butler, B. L., Binkowski, B. F., Machleidt, T., Kirkland, T. A., et al. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.5b00753 · Cited by 1,405 · see citing works

The global burden of hepatitis C

Lavanchy, D. (2009) · Liver International · doi:10.1111/j.1478-3231.2008.01934.x · Cited by 1,353 · see citing works

Adenosine receptors as drug targets — what are the challenges?

Chen, J., Eltzschig, H. K., & Fredholm, B. B. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd3955 · Cited by 899 · see citing works

Weight Gain Following Initiation of Antiretroviral Therapy: Risk Factors in Randomized Comparative Clinical Trials

Sax, P. E., Erlandson, K. M., Lake, J. E., McComsey, G. A., Orkin, C. M., Eßer, S., Brown, T. T., Rockstroh, J. K., Wei, X., Carter, C. C., et al. (2019) · Clinical Infectious Diseases · doi:10.1093/cid/ciz999 · Cited by 775 · see citing works

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, D., Christopoulos, A., & Sexton, P. M. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd4052 · Cited by 498 · see citing works

Discovery, characterization, and clinical development of the glucagon-like peptides

Drucker, D. J., Habener, J. F., & Holst, J. J. (2017) · Journal of Clinical Investigation · doi:10.1172/jci97233 · Cited by 418 · see citing works

The anti-inflammatory and immunological properties of GLP-1 Receptor Agonists

Bendotti, G., Montefusco, L., Lunati, M. E., Usuelli, V., Pastore, I., Lazzaroni, E., Assi, E., Seelam, A. J., El Essawy, B., Jang, J., et al. (2022) · Pharmacological Research · doi:10.1016/j.phrs.2022.106320 · Cited by 406 · see citing works

Asymmetric organocatalysis: an enabling technology for medicinal chemistry

Han, B., He, X., Liu, Y., He, G., Peng, C. Y., & Li, J. (2021) · Chemical Society Reviews · doi:10.1039/d0cs00196a · Cited by 405 · see citing works

Current Research on Opioid Receptor Function

Feng, Y., He, X., Yang, Y., Chao, D., Lazarus, L. H., & Xia, Y. (2012) · Current Drug Targets · doi:10.2174/138945012799201612 · Cited by 330 · see citing works

Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators

Kruegel, A. C., Gassaway, M. M., Kapoor, A., Váradi, A., Majumdar, S., Filizola, M., Javitch, J. A., & Sameš, D. (2016) · Journal of the American Chemical Society · doi:10.1021/jacs.6b00360 · Cited by 325 · see citing works

Quantitative Detection of <i>EGFR</i> Mutations in Circulating Tumor DNA Derived from Lung Adenocarcinomas

Taniguchi, K., Uchida, J., Nishino, K., Kumagai, T., Okuyama, T., Okami, J., Higashiyama, M., Kodama, K., Imamura, F., & Kato, K. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-1712 · Cited by 315 · see citing works

Molecular recognition of morphine and fentanyl by the human μ-opioid receptor

Zhuang, Y., Wang, Y., He, B., He, X., Zhou, X. E., Guo, S., Rao, Q., Yang, J., Liu, J., Zhou, Q., et al. (2022) · Cell · doi:10.1016/j.cell.2022.09.041 · Cited by 284 · see citing works

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

Conn, P. J., Lindsley, C. W., Meiler, J., & Niswender, C. M. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4308 · Cited by 259 · see citing works

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Wootten, D. L., Simms, J., Miller, L. J., Christopoulos, A., & Sexton, P. M. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1221585110 · Cited by 249 · see citing works

Crystal structure of the GLP-1 receptor bound to a peptide agonist

Jazayeri, A., Rappas, M., Brown, A., Kean, J., Errey, J. C., Robertson, N. J., Fiez-Vandal, C., Andrews, S. P., Congreve, M., Bortolato, A., et al. (2017) · Nature · doi:10.1038/nature22800 · Cited by 200 · see citing works

Ondansetron Clinical Pharmacokinetics

Roila, F., & Favero, A. D. (1995) · Clinical Pharmacokinetics · doi:10.2165/00003088-199529020-00004 · Cited by 175 · see citing works

Structure of an allosteric modulator bound to the CB1 cannabinoid receptor

Shao, Z., Yan, W., Chapman, K., Ramesh, K. K., Ferrell, A. J., Yin, J., Wang, X., Xu, Q., & Rosenbaum, D. M. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0387-2 · Cited by 174 · see citing works

New Promise and Opportunities for Allosteric Kinase Inhibitors

Lu, X., Smaill, J. B., & Ding, K. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201914525 · Cited by 170 · see citing works

Allosteric Methods and Their Applications: Facilitating the Discovery of Allosteric Drugs and the Investigation of Allosteric Mechanisms

Lu, S., Shen, Q., & Zhang, J. (2019) · Accounts of Chemical Research · doi:10.1021/acs.accounts.8b00570 · Cited by 166 · see citing works

Interdomain Communication in Hepatitis C Virus Polymerase Abolished by Small Molecule Inhibitors Bound to a Novel Allosteric Site

Marco, S. D., Volpari, C., Tomei, L., Altamura, S., Harper, S., Narjes, F., Koch, U., Rowley, M., Francesco, R. D., Migliaccio, G., et al. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m505423200 · Cited by 165 · see citing works

Organocatalytic Asymmetric Tandem Michael−Henry Reactions: A Highly Stereoselective Synthesis of Multifunctionalized Cyclohexanes with Two Quaternary Stereocenters

Tan, B., Chua, P. J., Li, Y., & Zhong, G. (2008) · Organic Letters · doi:10.1021/ol8007183 · Cited by 154 · see citing works

Benzimidazole Derivatives Bearing Substituted Biphenyls as Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase Inhibitors: Structure−Activity Relationship Studies and Identification of a Potent and Highly Selective Inhibitor JTK-109

Hirashima, S., Suzuki, T., Ishida, T., Noji, S., Yata, S., Ando, I., Komatsu, M., Ikeda, S., & Hashimoto, H. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm060269e · Cited by 150 · see citing works

Challenges for opioid receptor nomenclature: IUPHAR Review 9

Cox, B. M., Christie, M. J., Devi, L. A., Toll, L., & Traynor, J. R. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12612 · Cited by 146 · see citing works

Harnessing Allostery: A Novel Approach to Drug Discovery

Lu, S., Li, S., & Zhang, J. (2014) · Medicinal Research Reviews · doi:10.1002/med.21317 · Cited by 146 · see citing works

HETEROCYCLIC AROMATIC AMINE METABOLISM, DNA ADDUCT FORMATION, MUTAGENESIS, AND CARCINOGENESIS

Turesky, R. J. (2002) · Drug Metabolism Reviews · doi:10.1081/dmr-120005665 · Cited by 132 · see citing works

Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine

Brossi, A. (1990) · Journal of Medicinal Chemistry · doi:10.1021/jm00171a001 · Cited by 130 · see citing works

Prodrugs of triterpenoids and their derivatives

Zhou, M., Zhang, R., Wang, M., Xu, G., & Liao, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.03.005 · Cited by 119 · see citing works

CB1 Receptor Allosteric Modulators Display Both Agonist and Signaling Pathway Specificity

Baillie, G. L., Horswill, J. G., Anavi‐Goffer, S., Reggio, P. H., Bolognini, D., Abood, M. E., McAllister, S. D., Strange, P. G., Stephens, G. J., Pertwee, R. G., et al. (2012) · Molecular Pharmacology · doi:10.1124/mol.112.080879 · Cited by 113 · see citing works

Discovery of Conformationally Constrained Tetracyclic Compounds as Potent Hepatitis C Virus NS5B RNA Polymerase Inhibitors

Ikegashira, K., Oka, T., Hirashima, S., Noji, S., Yamanaka, H., Hara, Y., Adachi, T., Tsuruha, J.-I., Doi, S., Hase, Y., et al. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm0610245 · Cited by 112 · see citing works

Potential antiradical and alpha-glucosidase inhibitors from Ecklonia maxima (Osbeck) Papenfuss

Rengasamy, K. R. R., Aderogba, M. A., Amoo, S. O., Stirk, W. A., & Staden, J. V. (2013) · Food Chemistry · doi:10.1016/j.foodchem.2013.04.019 · Cited by 108 · see citing works

Identification and Characterization of an RNA-Dependent RNA Polymerase Activity within the Nonstructural Protein 5B Region of Bovine Viral Diarrhea Virus

Zhong, W., Gutshall, L. L., & Vecchio, A. M. D. (1998) · Journal of Virology · doi:10.1128/jvi.72.11.9365-9369.1998 · Cited by 108 · see citing works

Discovery and Preclinical Characterization of the Cyclopropylindolobenzazepine BMS-791325, A Potent Allosteric Inhibitor of the Hepatitis C Virus NS5B Polymerase

Gentles, R. G., Ding, M., Bender, J. A., Bergstrom, C. P., Grant-Young, K. A., Hewawasam, P., Hudyma, T. W., Martin, S. W., Nickel, A., Regueiro‐Ren, A., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm4016894 · Cited by 103 · see citing works

Discovery of Pyrano[3,4-b]indoles as Potent and Selective HCV NS5B Polymerase Inhibitors

Gopalsamy, A., Lim, K., Ciszewski, G. M., Park, K., Ellingboe, J. W., Bloom, J. D., Insaf, S. S., Upeslacis, J., Mansour, T. S., Krishnamurthy, G., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm0401255 · Cited by 97 · see citing works

A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1

Rettenmaier, T. J., Sadowsky, J., Thomsen, N. D., Chen, S. C., Doak, A. K., Arkin, M. R., & Wells, J. A. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1415365112 · Cited by 91 · see citing works

Development and Preliminary Optimization of Indole-N-Acetamide Inhibitors of Hepatitis C Virus NS5B Polymerase

Harper, S., Pacini, B., Avolio, S., Filippo, M. D., Migliaccio, G., Laufer, R., Francesco, R. D., Rowley, M., & Narjes, F. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm049122i · Cited by 84 · see citing works

Adenosine A2A receptor occupancy stimulates expression of proteins involved in reverse cholesterol transport and inhibits foam cell formation in macrophages

Reiss, A. B., Rahman, M. M., Chan, E. S. L., Montesinos, M. C., Awadallah, N. W., & Cronstein, B. N. (2004) · Journal of Leukocyte Biology · doi:10.1189/jlb.0204107 · Cited by 81 · see citing works

Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities

Khurana, L., Mackie, K., Piomelli, D., & Kendall, D. A. (2017) · Neuropharmacology · doi:10.1016/j.neuropharm.2017.05.018 · Cited by 79 · see citing works

Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: patent review (2015-2018)

Hussain, H., Green, I. R., Abbas, G., Adekenov, S. M., Hussain, W., & Ali, I. (2019) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2019.1655542 · Cited by 79 · see citing works

Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer

Dockery, L., Gunderson, C., & Moore, K. (2017) · OncoTargets and Therapy · doi:10.2147/ott.s114714 · Cited by 75 · see citing works

Tadalafil for the treatment of benign prostatic hyperplasia

Mónica, F. Z., & Nucci, G. D. (2019) · Expert Opinion on Pharmacotherapy · doi:10.1080/14656566.2019.1589452 · Cited by 75 · see citing works

Prediction of rodent carcinogenicity of aromatic amines: a quantitative structure-activity relationships model

Franke, R. (2001) · Carcinogenesis · doi:10.1093/carcin/22.9.1561 · Cited by 74 · see citing works

Principles of Kinase Allosteric Inhibition and Pocket Validation

Pan, Y., & Mader, M. M. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00073 · Cited by 71 · see citing works

Adenosine A2A receptor as potential therapeutic target in neuropsychiatric disorders

Domenici, M. R., Ferrante, A., Martire, A., Chiodi, V., Pepponi, R., Tebano, M. T., & Popoli, P. (2019) · Pharmacological Research · doi:10.1016/j.phrs.2019.104338 · Cited by 70 · see citing works

Discovery of (7R)-14-Cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic Acid (MK-3281), a Potent and Orally Bioavailable Finger-Loop Inhibitor of the Hepatitis C Virus NS5B Polymerase

Narjes, F., Crescenzi, B., Ferrara, M., Habermann, J., Colarusso, S., Ferreira, M. D. R. R., Stansfield, I., Mackay, A., Conte, I., Ercolani, C., et al. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm1013105 · Cited by 67 · see citing works

Along the allostery stream: Recent advances in computational methods for allosteric drug discovery

Ni, D., Chai, Z., Wang, Y., Li, M., Yu, Z., Liu, Y., Lu, S., & Zhang, J. (2021) · Wiley Interdisciplinary Reviews Computational Molecular Science · doi:10.1002/wcms.1585 · Cited by 67 · see citing works

Design, synthesis, and biological evaluation of nitroisoxazole-containing spiro[pyrrolidin-oxindole] derivatives as novel glutathione peroxidase 4/mouse double minute 2 dual inhibitors that inhibit breast adenocarcinoma cell proliferation

Liu, S., Zhao, Q., Peng, C. Y., Mao, Q., Wu, F., Zhang, F., Feng, Q., He, G., & Han, B. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113359 · Cited by 64 · see citing works

Evodiamine as an anticancer agent: a comprehensive review on its therapeutic application, pharmacokinetic, toxicity, and metabolism in various cancers

Panda, M., Tripathi, S. K., Zengin, G., & Biswal, B. K. (2022) · Cell Biology and Toxicology · doi:10.1007/s10565-022-09772-8 · Cited by 62 · see citing works

Asymmetric synthesis of tetrahydroisoquinoline-fused spirooxindoles as Ras-GTP inhibitors that inhibit colon adenocarcinoma cell proliferation and invasion

Zhao, Q., Peng, C. Y., Huang, H., Liu, S., Zhong, Y., Huang, W., He, G., & Han, B. (2018) · Chemical Communications · doi:10.1039/c8cc04732d · Cited by 60 · see citing works

Molecular insights into allosteric modulation of Class C G protein-coupled receptors

Leach, K., & Gregory, K. J. (2016) · Pharmacological Research · doi:10.1016/j.phrs.2016.12.006 · Cited by 59 · see citing works

Advances in indole-containing alkaloids as potential anticancer agents by regulating autophagy

Luo, M.-L., Huang, W., Zhu, H.-P., Peng, C. Y., Zhao, Q., & Han, B. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.112827 · Cited by 59 · see citing works

Design and Application of Chiral Bifunctional 4-Pyrrolidinopyridines: Powerful Catalysts for Asymmetric Cycloaddition of Allylic N-Ylide

Luo, Q.-Q., Tian, Z., Tang, J., Wang, J., Yin, T., Peng, C. Y., Zhan, G., & Han, B. (2022) · ACS Catalysis · doi:10.1021/acscatal.2c01924 · Cited by 58 · see citing works

Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase

Stansfield, I., Ercolani, C., Mackay, A., Conte, I., Pompei, M., Koch, U., Gennari, N., Giuliano, C., Rowley, M., & Narjes, F. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.12.068 · Cited by 52 · see citing works

Structural modifications of 2,3-indolobetulinic acid: Design and synthesis of highly potent α-glucosidase inhibitors

Khusnutdinova, E. F., Petrova, A. V., Hà, N. T. T., Anh, L. T. T., Thanh, T. N., Cham, B. T., Babkov, D. A., & Kazakova, O. B. (2019) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2019.102957 · Cited by 52 · see citing works

Residues within the Transmembrane Domain of the Glucagon-Like Peptide-1 Receptor Involved in Ligand Binding and Receptor Activation: Modelling the Ligand-Bound Receptor

Coopman, K., Wallis, R., Robb, G. R., Brown, A., WILKINSON, G. F., Timms, D. A., & Willars, G. B. (2011) · Molecular Endocrinology · doi:10.1210/me.2011-1160 · Cited by 51 · see citing works

Synthesis and Biological Evaluation of 2-Amino-3-(4-Chlorobenzoyl)-4-[N-(Substituted) Piperazin-1-yl]Thiophenes as Potent Allosteric Enhancers of the A1Adenosine Receptor

Romagnoli, R., Baraldi, P. G., Carriòn, M. D., Lopez-Cara, L. C., Cruz‐López, O., Iaconinoto, M. A., Preti, D., Shryock, J. C., Moorman, A. R., Vincenzi, F., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800586p · Cited by 50 · see citing works

Discovery of ( S )-2-Cyclopentyl- N -((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1 H -pyrrido[3,4- b ]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM)

Morris, L. C., Nance, K. D., Gentry, P. R., Days, E., Weaver, C. D., Niswender, C. M., Thompson, A. D., Jones, C. K., Locuson, C. W., Morrison, R. D., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm501375c · Cited by 49 · see citing works

Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase

Habermann, J., Capitò, E., Ferreira, M. D. R. R., Koch, U., & Narjes, F. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.12.039 · Cited by 47 · see citing works

Synergisms in alpha-glucosidase inhibition and antioxidant activity of Camellia sinensis L. Kuntze and Eugenia uniflora L. Ethanolic Extracts

Vinholes, J. R., & Vizzotto, M. (2017) · Pharmacognosy Research · doi:10.4103/0974-8490.197797 · Cited by 47 · see citing works

Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus

Zheng, X., Hudyma, T. W., Martin, S. W., Bergstrom, C. P., Ding, M., He, F., Romine, J. L., Poss, M. A., Kadow, J. F., Chang, C., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.03.067 · Cited by 45 · see citing works

Indole-Based Small Molecules as Potential Therapeutic Agents for the Treatment of Fibrosis

Qin, R., Zhao, Q., Han, B., Zhu, H.-P., Peng, C. Y., Zhan, G., & Huang, W. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.845892 · Cited by 43 · see citing works

Synthesis and evaluation of 2,3-indolotriterpenoids as new α-glucosidase inhibitors

Khusnutdinova, E. F., Smirnova, I. E., Kazakova, O. B., Petrova, A. V., Hà, N. T. T., & Viet, D. Q. (2017) · Medicinal Chemistry Research · doi:10.1007/s00044-017-1972-0 · Cited by 42 · see citing works

A Positive Allosteric Modulator of the Serotonin 5-HT2CReceptor for Obesity

Garcı́a-Cárceles, J., Decara, J. M., Vázquez‐Villa, H., Rodríguez, R., Codesido, E., Cruces, J., Brea, J. M., Loza, M. I., Alén, F., Botta, J. A., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00994 · Cited by 40 · see citing works

1423 INTERIM ANALYSIS OF AN INTERFERON (IFN)- AND RIBAVIRIN (RBV)-FREE REGIMEN OF DACLATASVIR (DCV), ASUNAPREVIR (ASV), AND BMS-791325 IN TREATMENT-NAIVE, HEPATITIS C VIRUS GENOTYPE 1-INFECTED PATIENTS

Everson, G. T., Sims, K., Rodriguez‐Torres, M., Hézode, C., Lawitz, E., Bourlière, M., Loustaud-Ratti, V., Rustgi, V., Schwartz, H., Tatum, H. A., et al. (2013) · Journal of Hepatology · doi:10.1016/s0168-8278(13)61422-1 · Cited by 37 · see citing works

Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R)

Méndez, M. M., Matter, H., Defoßa, E., Kurz, M. E., Lebreton, S., Li, Z., Lohmann, M., Löhn, M., Mors, H., Podeschwa, M. A. L., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01071 · Cited by 37 · see citing works

Predicted Mode of Binding to and Allosteric Modulation of the μ-Opioid Receptor by Kratom’s Alkaloids with Reported Antinociception In Vivo

Zhou, Y., Ramsey, S., Provasi, D., Daibani, A. E., Appourchaux, K., Chakraborty, S., Kapoor, A., Che, T., Majumdar, S., & Filizola, M. (2020) · Biochemistry · doi:10.1021/acs.biochem.0c00658 · Cited by 36 · see citing works

Learning About Allosteric Drugs and Ways to Design Them

Tan, Z. W., Tee, W.-V., & Berezovsky, I. N. (2022) · Journal of Molecular Biology · doi:10.1016/j.jmb.2022.167692 · Cited by 36 · see citing works

Pharmacology and clinical experience with alosetron

Camilleri, M. (2000) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.9.1.147 · Cited by 31 · see citing works

The Discovery of Pyrano[3,4‐b]indole‐Based Allosteric Inhibitors of HCV NS5B Polymerase with In Vivo Activity

LaPorte, M. G., Jackson, R. W., Draper, T. L., Gaboury, J. A., Galie, K., Herbertz, T., Hussey, A. R., Rippin, S. R., Benetatos, C. A., Chunduru, S. K., et al. (2008) · ChemMedChem · doi:10.1002/cmdc.200800168 · Cited by 29 · see citing works

Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase

Ding, M., He, F., Hudyma, T. W., Zheng, X., Poss, M. A., Kadow, J. F., Beno, B. R., Rigat, K. L., Wang, Y.-K., Fridell, R. A., et al. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.02.063 · Cited by 24 · see citing works

Protein tyrosine phosphatase 1B inhibitors from the fungus Malbranchea albolutea

Díaz-Rojas, M., Raja, H. A., González‐Andrade, M., Rivera‐Chávez, J., Rangel‐Grimaldo, M., Rivero‐Cruz, I., & Mata, R. (2021) · Phytochemistry · doi:10.1016/j.phytochem.2021.112664 · Cited by 22 · see citing works

The discovery and structure–activity relationships of pyrano[3,4-b]indole-based inhibitors of hepatitis C virus NS5B polymerase

Jackson, R. W., LaPorte, M. G., Herbertz, T., Draper, T. L., Gaboury, J. A., Rippin, S. R., Patel, R., Chunduru, S. K., Benetatos, C. A., Young, D. C., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.04.052 · Cited by 22 · see citing works

Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor

Romagnoli, R., Baraldi, P. G., Carriòn, M. D., Lopez-Cara, L. C., Salvador, M. K., Preti, D., Tabrizi, M. A., Moorman, A. R., Vincenzi, F., Borea, P. A., et al. (2013) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2013.07.002 · Cited by 19 · see citing works

Unconventional [2 + 3] Cyclization Involving [1,4]-Sulfonyl Transfer to Construct Polysubstituted Fluorazones as Inhibitors of Indoleamine 2,3-Dioxygenase 1

Xue Ming, T. A. N. G., Zhang, N., He, G., Li, C., Huang, W., Wang, X., Zhan, G., & Han, B. (2020) · Organic Letters · doi:10.1021/acs.orglett.0c02836 · Cited by 19 · see citing works

Winning the Arms Race by Improving Drug Discovery against Mutating Targets

Anderson, A. C. (2011) · ACS Chemical Biology · doi:10.1021/cb200394t · Cited by 16 · see citing works

Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: Improved drug-like properties through C-2 SAR in three sub-series

Beaulieu, P. L., Dansereau, N., Duan, J., Garneau, M., Gillard, J. R., McKercher, G., LaPlante, S. R., Lagacé, L., Thauvette, L., & Kukolj, G. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.02.003 · Cited by 15 · see citing works

Structure–activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A1 adenosine receptor

Romagnoli, R., Baraldi, P. G., Carriòn, M. D., Lopez-Cara, L. C., Cruz‐López, O., Salvador, M. K., Preti, D., Tabrizi, M. A., Shryock, J. C., Moorman, A. R., et al. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.11.044 · Cited by 14 · see citing works

Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters

Barresi, E., Giacomelli, C., Marchetti, L., Baglini, E., Salerno, S., Greco, G., Settimo, F. D., Martini, C., Trincavelli, M. L., & Taliani, S. (2020) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2020.1862103 · Cited by 14 · see citing works

Allosteric Modulators of Dopamine D2 Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis

Kaczor, A. A., Wróbel, T. M., & Bartuzi, D. (2022) · Molecules · doi:10.3390/molecules28010178 · Cited by 13 · see citing works

Phase II trial of CH5424802 (alectinib hydrochloride) for recurrent or refractory ALK-positive anaplastic large cell lymphoma: study protocol for a non-randomized non-controlled trial.

Nagai, H., Fukano, R., Sekimizu, M., Kada, A., Saito, A. M., Asada, R., & Mori, T. (2017) · PubMed Central · doi:10.18999/nagjms.79.3.407 · Cited by 11 · see citing works

Tadalafil treatment improves cardiac, renal and lower urinary tract dysfunctions in rats with heart failure

Mora, A. G., Andrade, D. R., Janussi, S., Gonçalves, T. T., Krikorian, K., Priviero, F. B. M., & Claudino, M. A. (2021) · Life Sciences · doi:10.1016/j.lfs.2021.120237 · Cited by 10 · see citing works

Design, Synthesis, and Biological Evaluation of Tetrahydro‐α‐carbolines as Akt1 Inhibitors That Inhibit Colorectal Cancer Cell Proliferation

Guo, L., He, X., Li, H., Zhao, Q., Li, D., Zhu, H., Zhang, Y., Zhan, G., & Huang, W. (2022) · ChemMedChem · doi:10.1002/cmdc.202200104 · Cited by 10 · see citing works

[Clinical, rheoencephalographic and ophthalmodynamographic double-blind studies of the effects of vincamine in the treatment of cerebrovascular diseases].

Kauchtschischvili, G., Nappi, G., & Bono, G. (1974) · PubMed · Cited by 5 · see citing works

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · see citing works

Organocatalytic Asymmetric Cycloaddition for the Construction of Chiral Indole‐Fused Medium‐ and Large‐Sized Rings

Lai, B., Zhang, H.-H., Yao, B.-X., Li, R., Ni, S., Dong, K., & Shi, F. J. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202507804 · Cited by 33 · see citing works

Organocatalytic asymmetric cascade bicyclization: access to chiral polycyclic bisindoles from 2-indolylmethanols and propargylic alcohols

Zhu, W.-R., Su, Q., Deng, X., Ouyang, Z.-L., Weng, J., & Lu, G. (2024) · Organic Chemistry Frontiers · doi:10.1039/d3qo01558k · Cited by 25 · see citing works

Visible-light-mediated substituent-controlled regiodivergent (2 + 2)/(3 + 2) cycloadditions for the synthesis of aza-analogs of β-lactam and γ-fused lactam derivatives

Zuo, W., Zhang, Y., Luo, Y., Li, X., Zhan, G., Zhou, J., Pang, Q., Yang, Q., & Han, B. (2024) · Organic Chemistry Frontiers · doi:10.1039/d4qo00584h · Cited by 14 · see citing works

Regio- and Enantioselective N -Heterocyclic Carbene-Catalyzed Annulation of Aminoindoles Initiated by Friedel–Crafts Alkylation

Dočekal, V., Niderer, Y., Kurčina, A., Cı́sařová, I., & Veselý, J. (2024) · Organic Letters · doi:10.1021/acs.orglett.4c02434 · Cited by 9 · see citing works

Catalyst-controlled regiodivergence and stereodivergence in formal cross-[4+2] cycloadditions: The unique effect of bismuth(III)

Hou, Q., Cai, C., Liu, S., Huang, W., Peng, C. Y., Zhan, G., & Han, B. (2025) · Science Advances · doi:10.1126/sciadv.adt5997 · Cited by 8 · see citing works

Enhanced Cytotoxicity and Antimelanoma Activity of Novel Semisynthetic Derivatives of Betulinic Acid with Indole Conjugation

Lombrea, A., Watz, C. G., Bora, L., Dehelean, C. A., Diaconeasa, Z. M., Dinu, Ş., Turks, M., Lugiņina, J., Peipiņš, U., & Danciu, C. (2023) · Plants · doi:10.3390/plants13010036 · Cited by 7 · see citing works

Diastereoselective radical cascade cyclization to access indole-fused diazepine derivatives

Wang, Y., Huang, X., Chen, J., Xu, J., & Song, Q. (2025) · Organic & Biomolecular Chemistry · doi:10.1039/d5ob00219b · Cited by 7 · see citing works

Enantioselective Synthesis of N-Substituted Indoles with α,β-Stereocenters via Sequential Aza-Piancatelli/Cyclization Reactions

Xie, K., Nie, X., Zhou, P., Tang, Y., & Cai, Y. (2025) · Organic Letters · doi:10.1021/acs.orglett.5c01381 · Cited by 6 · see citing works

1,3-Dipolar Cycloaddition and Mannich Reactions of Alkynyl Triterpenes: New Trends in Synthetic Strategies and Pharmacological Applications

Petrova, A. V., & Kazakova, O. B. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26094329 · Cited by 5 · see citing works

Asymmetric synthesis of quinolinone-based polycyclic indoles through [1,3]-rearrangement/cyclization reaction

Xu, F., Xiong, Z., Qin, W., Yao, W., & Wang, Z. (2025) · Chemical Communications · doi:10.1039/d5cc00612k · Cited by 5 · see citing works

Indole therapeutics: Latest FDA updates, ongoing trials, and future directions

Butt, N.-U.-H., & Baytaş, S. N. (2025) · Drug Discovery Today · doi:10.1016/j.drudis.2025.104471 · Cited by 4 · see citing works

Organocatalytic Asymmetric Cycloaddition for the Construction of Chiral Indole‐Fused Medium‐ and Large‐Sized Rings

Lai, B., Zhang, H.-H., Yao, B.-X., Li, R., Ni, S., Dong, K., & Shi, F. J. (2025) · Angewandte Chemie · doi:10.1002/ange.202507804 · Cited by 4 · see citing works

Cu-catalyzed reductive Friedel-Crafts alkylation of indoles with ketones for one-pot synthesis of 3-substituted indoles

Wang, W., & Mao, Z. (2025) · Journal of Organometallic Chemistry · doi:10.1016/j.jorganchem.2025.123513 · Cited by 3 · see citing works

Design, synthesis, and antiproliferative efficacy of an innovative series of triazino[5,6-b]indole derivatives targeting EGFR, CD1, Hsp90, PI3K, and ERK/AKT as key molecular targets in cancer therapy

Ezz-ElDien, E. S., Badawi, W. A., El‐Atawy, M. A., Elhag, M., Hamed, E. A., Ahmed, H. A., Jaremko, M., Emwas, A.-H. M., Okda, T. M., El-Readi, M. Z., et al. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118263 · Cited by 2 · see citing works

PTP1B Inhibitors for Type 2 Diabetes: From Natural Products, Synthetic Inhibitors, and Multi-Target Drug Design Strategies to Clinical Translation

Joshi, P., Mazumder, A., Pentela, B., & Debnath, A. (2026) · Current Drug Targets · doi:10.2174/0113894501447162260311053819 · Cited by 2 · see citing works

Discovery of tri(indolyl)methanes as potent and selective inhibitors against human carboxylesterase 2

Li, W., Mu, J., Wang, A., Su, Q.-L., Li, M., Lü, C., & Zou, L. (2025) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2025.141868 · Cited by 2 · see citing works

Bis‐Tetrasubstituted Centers Forming Formal [3 + 3] Cycloaddition Reaction via Bifunctional Organocatalysis: Synthesis of Spiro‐Oxindoles

Xiong, Y., Liu, J., Ma, Y., Jiang, Z., Ge, Y., & Tang, J. (2025) · European Journal of Organic Chemistry · doi:10.1002/ejoc.202500324 · Cited by 2 · see citing works

A new synthetic approach to the 3,4-dihydro-1 H -[1,4]oxazino[4,3- a ]indole system from ethyl 1 H -indole-2-carboxylates and activated glycerol carbonate

Zagorskytė, I., Arbačiauskienė, E., Račkauskienė, G., Belyakov, S., Bieliauskas, A., Rollin, P., & Šačkus, A. (2025) · RSC Advances · doi:10.1039/d5ra02996a · Cited by 2 · see citing works

A Build, Couple, Pair (B/C/P) Strategy in the Synthesis of Diindole Fused Diazamacrocycles: An Attempt to a Green Synthetic Approach

Mangali, R. (2025) · ACS Omega · doi:10.1021/acsomega.5c08238 · Cited by 2 · see citing works

Photochemical Synthesis of Fused Indole Derivatives

Fisyuk, A. S., Samsonenko, A. L., Kostyuchenko, A. S., Zheleznova, T. Y., Uliankin, E. B., Shuvalov, V. Y., Shatsauskas, A. L., & Chernenko, S. А. (2025) · Synthesis · doi:10.1055/a-2510-5450 · Cited by 1 · see citing works

Photoinduced cross-coupling of indoles with ICF 2 SO 2 Ph promoted by DABSO

Liang, J., Long, X., Zhang, H., Zhang, J., Wang, P., Yingshu, X., Yao, Q., & He, C. (2026) · Organic Chemistry Frontiers · doi:10.1039/d6qo00147e · Cited by 1 · see citing works

Construction of the Akuammiline Alkaloid Core Structure via Stereoselective E-Ring Formation

Hashimoto, N., Taguchi, J., Kasagi, T., Arichi, N., Inuki, S., & Ohno, H. (2024) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.4c01105

Conjugation of Triterpenic Acids with 3-Aminoquinuclidine Moiety: An Approach to Acetylcholinesterase Mixed or Uncompetitive Type Inhibitors

Petrova, A. V., Nguyen, H. T., Zueva, I. V., Petrov, K. A., Lobov, A. N., & Kazakova, O. B. (2024) · Molecules · doi:10.3390/molecules30010095

Catalytic Enantioselective Synthesis of Chiral Indole‐Fused Medium and Large Rings: A Burgeoning Field

Li, H., & Liu, F. (2026) · European Journal of Organic Chemistry · doi:10.1002/ejoc.70700

Rational design of allosteric modulators: Challenges and successes

Chatzigoulas, A., & Cournia, Z. (2021) · Wiley Interdisciplinary Reviews Computational Molecular Science · doi:10.1002/wcms.1529 · Cited by 87 · see citing works

Harnessing Allostery: A Novel Approach to Drug Discovery

Lu, S., Li, S., & Zhang, J. (2014) · Medicinal Research Reviews · doi:10.1002/med.21317 · Cited by 146 · see citing works

Allosteric Modulator Discovery: From Serendipity to Structure-Based Design

Lu, S., He, X., Ni, D., & Zhang, J. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01749 · Cited by 176 · see citing works

Allosteric Modulators

Lu, S., & Zhang, J. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-409547-2.12324-8 · Cited by 9 · see citing works

Call for Papers: Allosteric Modulators in Drug Discovery

Blanco, M.-J., Cournia, Z., Huang, R., & Siew, C. Y. (2026) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6c00260